He was born on 19 June 1783 in Schloß Neuhaus (now part of Paderborn).

As a pharmacist's apprentice in Paderborn, he was the first to isolate morphine from opium. He called the isolated alkaloid "morphium" after the Greek god of dreams, Morpheus. It was not only the first alkaloid to be extracted from opium, but the first ever alkaloid to be isolated from any plant. Thus he became the first person to isolate the active ingredient associated with a medicinal plant or herb.

In the years following, he investigated the effects of morphine. However, it only became widely used after 1815. In 1809, Sertürner opened his first own pharmacy in Einbeck. In 1822, he bought the main pharmacy in Hamelin (Rathaus Apotheke), where he worked until his death in 1841.

Friedrich, C; Seidlein, HJ (May 1984). "The history of pharmaceutical science. 12. The importance of the discovery of morphine in the development of pharmaceutical science" [The history of pharmaceutical science. 12. The importance of the discovery of morphine in the development of pharmaceutical science]. Die Pharmazie (in German) 39 (5): 340–5. ISSN0031-7144. PMID6382346.